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. 2020 May 5;117(20):10688–10698. doi: 10.1073/pnas.1919408117

Table 1.

Binding affinities to PKC δ and PKC βI for tigliane, ingenane, and bryostatin analogs and prodrugs

PKC binding affinity, Ki
4 (parent) 0.5 nM, 1.4 nM*
 6a >2.5 µM
 6b >2.5 µM, >2.5 µM*
 6c >2.5 µM
 6d >2.5 µM, >0.5 µM*
 6e 380 nM
 6f >2.5 µM
9 (parent) 1.1 nM, 0.85 nM*
 7 >2.5 µM, >2.5 µM*
1 (parent) 1.1 nM, 2.2 nM*
 8a >1 µM
 8b >5 µM
 8c 308 nM
 8d >5 µM
 8e >5 µM

Ki values are from a heterogeneous competitive binding assay against [3H]-phorbol dibutyrate.

*

Binding affinity to PKC δ and βI, respectively.

Binding affinity to PKC δ.

Binding affinity to PKC βI.